Objectives
This practical/hands-on course is specifically designed for personnel in the pharmaceutical and biotechnology industries and contract research organizations (CROs), who need to understand:
- Drug transporters as an emerging field of science – why and why now?
- Molecular mechanisms and role in ADME
- Extended clearance classification system [ECCS] and its utility in defining new molecular entity drug transporter-related clearance
- Intestinal transporter organ expression and their impacts on drug absorption and disposition
- Blood brain barrier transporters and their impact on brain delivery
- Renal transporters and their impact on drug renal elimination
- Hepatobiliary transporters and their impact on drug hepatic uptake, liver concentration and biliary elimination
- Impact of disease states on transporter expression and function.
- Assessment of the impact of disease state, age, and pregnancy on transporter expression and function.
- The in vitro and in vivo tools to assess transporter contributions to drug disposition.
- Introduction to the US FDA and EMA Transporter DDI regulations and case studies.
- Transporter-enzyme interplay and the extended clearance concepts
- Static models to predict transporter mediated DDI: Emphasis on hepatic and renal DDI prediction
- Dynamic models to predict complex DDI: Introduction to physiologically based pharmacokinetics modeling (PBPK) utility in DDI predictions.
- The workshop will also include a hands-on session that aims at improving your ability to apply these strategies to medicinal chemistry for hit selection, lead optimization, development candidate selection and designing clinical plans for the labels.
Who should attend this course?
100% of the attendees in the 2015 workshop agreed that he/she would recommend the course to others who want to learn more about transporters
The interest in the field of transporters and their impact on drug absorption and disposition has been re-invigorated due to recent FDA and EMA guidance on approaches to assess transporter mediated DDI liabilities for NME. Therefore, this course is designed to serve a variety of scientific communities.
- Senior level managers and industrial, biopharmaceutics and contract research organization (CRO) scientists desiring to understand the overall role of transporters in drug absorption and disposition, subsequently to design compounds with transporter interaction for the optimization of PK/safety profiles.
- Regulatory scientists who needs to understand recent FDA and EMA regulations on drug transporters DDI.
- Scientists who develop and conduct in vitro transporter studies and/or in vivo pharmacokinetic studies.
- Registrants should possess a basic knowledge of drug discovery and development.
What are the benefits?
By the end of workshop, students will understand the role of transporters in drug disposition, physicochemical properties needed for NMEs to avoid or be substrates for various transporters. Also how to interpret data generated in in vitro/in vivo settings. It will also provide a better understanding of the recent FDA and EMA regulations and how to put them in context from drug development setting. This course will also provide an overview on approaches to characterize the potential for transporters mediated drug-drug interaction using both static and dynamic mechanistic/ whole-body PBPK modeling.
How are the workshops run?
The course is composed of lectures – delivered by leading experts in the field of transporters and provides in-depth overview of various topics presented. It is also mixed with a small group exercises with an expert tutor, where students will be presented with industry relevant examples to integrate acquired knowledge.